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Ebastine

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Chemical Structure| 90729-43-4 同义名 : LAS-W 090;RP64305;Kestin;Evastel;Busidril;Bactil;Ebatrol;Aleva;Ebastel;Kestine;Brand name: Evastin
CAS号 : 90729-43-4
货号 : A124731
分子式 : C32H39NO2
纯度 : 98%
分子量 : 469.658
MDL号 : MFCD00865661
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 7 mg/mL(14.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

无水乙醇: 55 mg/mL(117.11 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 6 mg/mL clear

PO 0.5% CMC-Na 38 mg/mL suspension

生物活性
靶点

  • H1 receptor
描述 Ebastine is a second-generation histamine H1 receptor antagonist that is used to attenuate allergic inflammation. Ebastine was shown to significantly increase the proliferation of HFDPC (human follicle dermal papilla cells)[3]. Ebastine is a well-established second generation oral H1-antihistamine that is administered once daily at a dose of 10 - 20 mg and is available both as a standard tablet and as a fast-dissolving tablet that disintegrates in the mouth. Ebastine has been shown to relieve symptoms in patients with allergic rhinitis or urticaria in multiple clinical trials. Ebastine is generally well tolerated at recommended doses[4]. Pooled data from clinical efficacy trials of ebastine 1 - 30 mg/day administered for 2 - 3 weeks showed no clinically relevant cardiac effects as assessed by serial electrocardiographs and Holter monitoring[5]. Ebastine 10 mg daily is a well tolerated and effective treatment for allergic rhinitis and chronic idiopathic urticaria[6]. Ebastine 20 mg/day is indicated in patients with moderate and severe allergic symptoms, it has no relevant effects on the psychomotor performance[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01144832 Irritable Bowel Syndrome Phase 4 Completed - Belgium ... 展开 >> University hospitals Leuven Leuven, Vlaams-Brabant, Belgium, 3000 收起 <<
NCT01940393 Urticaria Phase 4 Completed - Colombia ... 展开 >> Medellin Medellin, Antioquia, Colombia 收起 <<
NCT02065440 Cough Not Applicable Unknown - Korea, Republic of ... 展开 >> Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, Seoul Metropolitan Government, Seoul National University Boramae Medical Center Seoul, Dongjak-Gu, Korea, Republic of, 156-707 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.29mL

4.26mL

2.13mL
参考文献

[1]Rapolu R, Pandey AK, et al. A novel UV degradation product of Ebastine: isolation and characterization using Q-TOF, NMR, IR and computational chemistry. J Pharm Biomed Anal. 2015 Mar 25;107:488-94.

[2]Ko CM, Ducic I, et al. Suppression of mammalian K+ channel family by ebastine. J Pharmacol Exp Ther. 1997 Apr;281(1):233-44.

[3]Tsai FM, Li CH, Wang LK, Chen ML, Lee MC, Lin YY, Wang CH. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503

[4]Sastre J. Ebastine in the Treatment of Allergic Rhinitis and Urticaria: 30 Years of Clinical Studies and Real-World Experience. J Investig Allergol Clin Immunol. 2020;30(3):156-168

[5]Moss AJ, Chaikin P, Garcia JD, Gillen M, Roberts DJ, Morganroth J. A review of the cardiac systemic side-effects of antihistamines: ebastine. Clin Exp Allergy. 1999 Jul;29 Suppl 3:200-5

[6]Hurst M, Spencer CM. Ebastine: an update of its use in allergic disorders. Drugs. 2000 Apr;59(4):981-1006

[7]Van Cauwenberge P, De Belder T, Sys L. A review of the second-generation antihistamine ebastine for the treatment of allergic disorders. Expert Opin Pharmacother. 2004 Aug;5(8):1807-13